The present invention relates to 4-(hydroxydiphenylmethyl)-1-piperidylphenylalkane derivatives and their use as antihistamines.
It is known that 4-diphenylmethylpiperidine derivatives can be used as antihistamines. A corresponding action has been described for piperidinobutanols and 1-piperidinopropanols in DE 2,506,770, DE 2,303,305, DE 2,303,306, DE 2,503,362 and DE 3,007,498.
.alpha.-[4-(1,1-Dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidin obutanol, INN terfenadine, is used in therapy as an antihistamine.
Many substances based on .alpha.,.alpha.-diphenyl-4-piperidylmethanol, including some with pharmaceutical activity, have been described. U.S. Pat. No. 3,014,037 and U.S. Pat. No. 3,068,237 describe these substances as papaverine-type spasmolytics with musculotropic activity, and as substances having antisecretory activity. It has also been reported that the barbiturate sleeping time of mammals is prolonged.
It has been reported that .alpha.,.alpha.-diphenyl-4-piperidylmethanol derivatives and compounds that are closely chemically related display a cerebral vasodilating action, i.e., musculotropic spasmolytic action can be detected in this vascular region. Chem. Pharm. Bull. 35, 4637-4641 (1987).